High-throughput screening method of inhibitors that block the interaction between 2 helical regions of HIV-1 gp41

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Title
High-throughput screening method of inhibitors that block the interaction between 2 helical regions of HIV-1 gp41
Author(s)
B S Jin; W K Lee; K Ahn; Myung Kyu Lee; Y G Yu
Bibliographic Citation
Journal of Biomolecular Screening, vol. 10, no. 1, pp. 13-19
Publication Year
2005
Abstract
The HIV-1 envelope glycoprotein transmembrane subunit, gp41, mediates the fusion of viral and target cell membranes. The 2 helical regions in the ectodomain of gp41, the N-helix and the C-helix, form a helical bundle complex that has been suggested as a fusion-active conformation. Previously, an enzyme-linked immunosorbent assay (ELISA) method had been established to measure the interaction of 2 helical regions of gp41. In this study, the ELISA method was modified to apply high-throughput screening (HTS) of an organic compound library. A few compounds had been identified to prevent the interaction between 2 helical regions of gp41, and they were further shown to inhibit the gp41-mediated viral infection. In addition, they specifically quenched the fluorescence of tryptophan in the N-helix region, indicating that these compounds bound to the N-helix rather than the C-helix of gp41. These results suggested that this assay method targeting gp41 could be used for HTS of HIV fusion inhibitors.
Keyword
gp41HIV-1InhibitorMembrane fusionScreening
ISSN
1087-0571
Publisher
Sage
DOI
http://dx.doi.org/10.1177/1087057104269726
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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